GDC-0623 (RG 7421) is a potent, ATP-uncompetitive inhibitor of MEK1 (Ki=0.13 nM, +ATP), and displays 6-fold weaker potency against HCT116 (KRAS (G13D), EC50=42 nM) versus A375 (BRAF, EC50=7 nM).
性状
Solid
IC50 & Target[1][2]
MEK1
0.13 nM (Ki, +ATP)
体外研究(In Vitro)
GDC-0623 (RG 7421) and G-573 are able to prevent MEK phosphorylation by CRAF 体外研究, and able to block MEK phosphorylation by BRAF(V600E). GDC-0623 (RG 7421) is potent, ATP-uncompetitive inhibitors of MEK1 but shows distinct shifts in cellular activity compared with the other two inhibitors, only 6-fold half-maximum effective concentration (EC50) decreases.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
GDC-0623 (RG 7421) (40 mg/kg, p.o.) shows percent tumour growth inhibition (%TGI) in MiaPaCa-2 xenograft model. GDC-0623 (RG 7421) and G-573 show superior antitumour activity compared to GDC-0623 (RG 7421) in all three KRAS models.
Medlife has not independently confirmed the accuracy of these methods. They are for reference only.